β glucuronidase in 1

β-Glucuronidase-IN-1 is an E. coli β-glucuronidase (β-glucuronidase) inhibitor with a potent, selective, non-competitive, and orally active IC50 and Ki value of 283 nM and 164 nM, respectively, against E. coli β-glucuronidase.

β-Glucuronidase hCAII-IN-2 (Compound 12e) effectively inhibits β-glucuronidase and human Carbonic Anhydrase II (hCA II) with IC50 values of 440.1 μM and 4.91 μM, respectively [1].

EcGUS-IN-1 (Compound E-9) is a non-competitive inhibitor of β-glucuronidase, featuring an IC50 value of 2.68 μM and a Ki value of 1.64 μM. This compound effectively mitigates gastrointestinal adverse events (GIAE) associated with Escherichia coli infections by inhibiting the activity of E. coli β-glucuronidase.

HPSE1-IN-1 (compound 16) functions as a selective Heparanase-1 (HPSE1) inhibitor, displaying moderate activity against exo-β-d-glucuronidase (GUSβ) and glucocerebrosidase (GBA) [1].

HPSE1-IN-2 (compound 2) functions as an inhibitor of Heparanase-1 (HPSE1) while concurrently inhibiting exo-β-d-glucuronidase (GUSβ) and glucocerebrosidase (GBA) activities [1].

hCAII-IN-4 (Compound 12j) is a potent inhibitor of human carbonic anhydrase II (hCA II) with an IC50 of 7.78 μM, and also inhibits β-glucuronidase with an IC50 of 773.9 μM [1].

β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20), an auristatins-glucuronide conjugate, exhibits in vitro antiproliferative effects on cancer cells, both β-glucuronidase pretreated and untreated, with an IC50 range of 5.7 nM to 9.7 nM. Demonstrating powerful antitumor efficacy in an HCT-116 xenograft mouse model, this compound does not induce side effects [1].